Camicinal free base

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319727

CAS#: 923565-21-3 (free base)

Description: Camicinal, also known as GSK962040, is a selective motilin receptor agonist and effective as a stimulant of human and rabbit gastrointestinal motility. Camicinal represents a new opportunity as a treatment in a clinical area in need of new agents.

Chemical Structure

Camicinal free base

CAS# 923565-21-3 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 319727
Name: Camicinal free base
CAS#: 923565-21-3 (free base)
Chemical Formula: C25H33FN4O
Exact Mass: 424.26
Molecular Weight: 424.564
Elemental Analysis: C, 70.73; H, 7.83; F, 4.47; N, 13.20; O, 3.77

Price and Availability

Size	Price	Availability	Quantity
1g	USD -1
2g	USD -1
5g	USD -1
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 923565-21-3 (free base) 923565-22-4 (HCl)

Synonym: GSK962040; GSK-962040; GSK 962040; Camicinal.

IUPAC/Chemical Name: (S)-1-(4-((3-fluorophenyl)amino)piperidin-1-yl)-2-(4-((3-methylpiperazin-1-yl)methyl)phenyl)ethan-1-one

InChi Key: RZKDEGZIFSJVNA-IBGZPJMESA-N

InChi Code: InChI=1S/C25H33FN4O/c1-19-17-29(14-11-27-19)18-21-7-5-20(6-8-21)15-25(31)30-12-9-23(10-13-30)28-24-4-2-3-22(26)16-24/h2-8,16,19,23,27-28H,9-15,17-18H2,1H3/t19-/m0/s1

SMILES Code: C[C@H]1CN(CC2=CC=C(CC(N3CCC(NC4=CC=CC(F)=C4)CC3)=O)C=C2)CCN1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 424.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Barshop K, Kuo B. The investigational drug camicinal for the treatment of gastroparesis. Expert Opin Investig Drugs. 2015 Jan;24(1):133-140. Epub 2014 Oct 24. PubMed PMID: 25341626.

2: Broad J, Góralczyk A, Mannur K, Dukes GE, Sanger GJ. Drugs acting at 5-HT4 , D2 , motilin, and ghrelin receptors differ markedly in how they affect neuromuscular functions in human isolated stomach. Neurogastroenterol Motil. 2014 Jun;26(6):851-61. doi: 10.1111/nmo.12338. Epub 2014 Apr 20. PubMed PMID: 24750304.

3: Sanger GJ. Ghrelin and motilin receptor agonists: time to introduce bias into drug design. Neurogastroenterol Motil. 2014 Feb;26(2):149-55. doi: 10.1111/nmo.12300. Review. PubMed PMID: 24438586.

4: Sanger GJ, Wang Y, Hobson A, Broad J. Motilin: towards a new understanding of the gastrointestinal neuropharmacology and therapeutic use of motilin receptor agonists. Br J Pharmacol. 2013 Dec;170(7):1323-32. doi: 10.1111/bph.12075. PubMed PMID: 23189978; PubMed Central PMCID: PMC3838679.

5: Depoortere I. Can small non-peptide motilin agonists force a breakthrough as gastroprokinetic drugs? Br J Pharmacol. 2012 Oct;167(4):760-2. doi: 10.1111/j.1476-5381.2012.02046.x. PubMed PMID: 22616752; PubMed Central PMCID: PMC3575776.

6: Broad J, Mukherjee S, Samadi M, Martin JE, Dukes GE, Sanger GJ. Regional- and agonist-dependent facilitation of human neurogastrointestinal functions by motilin receptor agonists. Br J Pharmacol. 2012 Oct;167(4):763-74. doi: 10.1111/j.1476-5381.2012.02009.x. PubMed PMID: 22537158; PubMed Central PMCID: PMC3575777.

7: Leming S, Broad J, Cozens SJ, Otterson M, Winchester W, Lee K, Dukes GE, Sanger GJ. GSK962040: a small molecule motilin receptor agonist which increases gastrointestinal motility in conscious dogs. Neurogastroenterol Motil. 2011 Oct;23(10):958-e410. doi: 10.1111/j.1365-2982.2011.01770.x. Epub 2011 Sep 5. PubMed PMID: 21895874.

8: Tack J, Janssen P. Emerging drugs for functional dyspepsia. Expert Opin Emerg Drugs. 2011 Jun;16(2):283-92. doi: 10.1517/14728214.2011.558502. Epub 2011 Mar 17. Review. PubMed PMID: 21413902.

9: Sanger GJ, Westaway SM, Barnes AA, Macpherson DT, Muir AI, Jarvie EM, Bolton VN, Cellek S, Näslund E, Hellström PM, Borman RA, Unsworth WP, Matthews KL, Lee K. GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterol Motil. 2009 Jun;21(6):657-64, e30-1. doi: 10.1111/j.1365-2982.2008.01270.x. PubMed PMID: 19374732.

10: Westaway SM, Brown SL, Fell SC, Johnson CN, MacPherson DT, Mitchell DJ, Myatt JW, Stanway SJ, Seal JT, Stemp G, Thompson M, Lawless K, McKay F, Muir AI, Barford JM, Cluff C, Mahmood SR, Matthews KL, Mohamed S, Smith B, Stevens AJ, Bolton VJ, Jarvie EM, Sanger GJ. Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-pi peridinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. J Med Chem. 2009 Feb 26;52(4):1180-9. doi: 10.1021/jm801332q. PubMed PMID: 19191554.

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